Rhubarb is one of the commonly used drugs in clinic, which is a good medicine for purging fire and laxative, cooling blood and detoxification. This paper summarizes the effective components of anthraquinones, anthrones, rhein, emodin and chrysophanol. In clinical application, rhubarb and its drug pairs have different mechanisms in the treatment of various diseases. It has pharmacological effects such as regulating gastrointestinal tract, anti-tumor, anti-fibrosis, anti-inflammation and anti-oxidation, involving Wnt1/β-catenin, AMPK/TXNIP/NLRP3, TLR4/NF-κB/c-myc and other signaling pathways. In clinical application, rhubarb is often combined with Danshen, Taoren, Huanglian, Huangqi, Mahuang, Fuzi and other drugs, which has a certain effect on chronic kidney disease, adenomyosis, diabetes, pneumonia and other diseases. According to the different processing methods, the pharmacological effects of rhubarb change with the content of anthraquinone glycosides and monomer tannins. Modern research shows that the chemical composition of rhubarb before and after compatibility has a significant change. When the ratio of rhubarb to Salvia miltiorrhiza, Gardenia jasminoides, Centella asiatica, and Astragalus is 1∶2, 1∶1, 1∶5, 1∶1, respectively, it can maximize the drug efficacy, reduce toxic and side effects, and improve the effectiveness and safety of medication. This article focuses on the pharmacological effects of rhubarb and its compatibility research in network pharmacology, clinical compatibility application, and chemical composition changes before and after compatibility, in order to provide reference for the further development and utilization of rhubarb and its drug pairs, in order to better play the clinical value of traditional Chinese medicine rhubarb.